Fevipiprant
Based on 1 publication(s) in Google Scholar
Fevipiprant (QAW039, NVP-QAW039) is s an orally active, selective, reversible prostaglandin D2 (DP2) receptor antagonist with an Kd value of 1.14 nM. Fevipiprant has the potential for the research of bronchial asthma.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.38%
- CAS No.: 872365-14-5
- Formule: C19H17F3N2O4S
- Masse moléculaire:426.41
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Fevipiprant
More
Activité biologique
|
DP2 1.14 nM (Kd) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57Bl/6 mice[3]
-
Dosage:10 mg/kg
-
Administration:In the drinking water
-
Result:Efficiently reduced CaCl2-induced AAA formation with diminished elastin degradation, aortic macrophage infiltration, MPO accumulation and MCP-1 expression.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 872365-14-5
-
Appearance Solid
-
Masse moléculaire 426.41
-
Formule C19H17F3N2O4S
-
Color White to off-white
-
SMILES
O=C(O)CC1=C(C)N(CC2=CC=C(S(=O)(C)=O)C=C2C(F)(F)F)C3=NC=CC=C31
-
Synonyms
QAW039; NVP-QAW039
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Int J Mol Sci
Prostaglandin D₂ Induces Ca2+ Sensitization of Contraction without Affecting Cytosolic Ca2+ Level in Bronchial Smooth Muscle. [Abstract]2018 Oct 5;19(10). pii: E3036. PMID: 30301147
Solvant et solubilité
DMSO : ≥ 32 mg/mL (75.05 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
-
Fiche technique (280 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instruction de manipulation (2659 KB)
Références
[1]. Brightling C, et al. The pharmacology of the prostaglandin D2 receptor 2 (DP2) receptor antagonist, fevipiprant. Pulm Pharmacol Ther. 2021 Jun;68:102030. [Content Brief]
[2]. Lee HY, et al. Blockade of thymic stromal lymphopoietin and CRTH2 attenuates airway inflammation in a murine model of allergic asthma. Korean J Intern Med. 2020 May;35(3):619-629. [Content Brief]
[3]. Weintraub NL, et al. Role of prostaglandin D2 receptors in the pathogenesis of abdominal aortic aneurysm formation. Clin Sci (Lond). 2022 Mar 18;136(5):309-321. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3452 mL | 11.7258 mL | 23.4516 mL | 58.6290 mL |
| 5 mM | 0.4690 mL | 2.3452 mL | 4.6903 mL | 11.7258 mL | |
| 10 mM | 0.2345 mL | 1.1726 mL | 2.3452 mL | 5.8629 mL | |
| 15 mM | 0.1563 mL | 0.7817 mL | 1.5634 mL | 3.9086 mL | |
| 20 mM | 0.1173 mL | 0.5863 mL | 1.1726 mL | 2.9315 mL | |
| 25 mM | 0.0938 mL | 0.4690 mL | 0.9381 mL | 2.3452 mL | |
| 30 mM | 0.0782 mL | 0.3909 mL | 0.7817 mL | 1.9543 mL | |
| 40 mM | 0.0586 mL | 0.2931 mL | 0.5863 mL | 1.4657 mL | |
| 50 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1726 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3909 mL | 0.9772 mL |